【作者】 季崇敏； 吴伟； 徐惠南；

【Author】 Chongmin Ji, Wei Wu*, Huinan Xu (Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, China)

【机构】 复旦大学药学院药剂教研室；

【摘要】 目的以吲哚美辛为模型药制备一种新型pH-酶双重促发的结肠定位释药小丸,考察体外释药行为,评价其结肠靶向性。方法采用流化床对空白丸芯喷液上药制备载药丸芯;采用流化包衣技术分别以4%(w/w)瓜尔胶的醇/水混悬液和10%(w/w)EudrgitFS30D水溶液对载药丸芯进行喷液包衣;体外考察影响药物释放的因素。结果外衣膜Eudrgit FS30D增重30%即可保护药物在0.1mol/LHCl和pH6.8PBS中至少8h不释放,而在pH7.4PBS中1h释药完全。随着包衣厚度的增加,瓜尔胶延缓药物释放的作用增强。当瓜尔胶增重44%即可在Eudragit FS30D溶解后继续保护药物不释放,最终控制药物在进入结肠前的释放量小于8%,而进入结肠后在酶促发下,2h的释药量达80%。结论Eudragit FS30D/瓜尔胶双层包衣小丸可将绝大部分的药物运送至结肠释放,因此具有良好的结肠定位释药特性。更多还原

【Abstract】 OBJECTIVE To develope a novel pH- , enzyme- double triggered colon-specific delivery pellets of indomethacin and investigate the release characteristics of them in vitro. METHODS In fluidized bed coater, drug loaded cores were prepared by spraying drug-binder suspension onto nonpareil, and Eudrgit FS30D/guar gum doubled coated pellets were prepared by spraying a dispersion of guar gum (4% w/w) and a aqueous dispersion of Eudragit FS30D (10% w/w) respectively. The factors on drug release were investigated. RESULTS The coat weight up to 30%, Eudragit FS30D can prevent drug from releasing within at least 8 h both in 0.1mol/L HCl and pH6.8PBS, however drug would release completely within 1 h once the Eudragit FS30D coated pellets came into pH7.4PBS. The effect of delaying drug release by guar gum was intensified with increasing coat weight of guar gum. Guar gum coating with 44% coat weight gain can continually protect drug and the release of drug was less than 8% before the colon, but the release amounted to 80% within 2 h in the colon. CONCLUSION Eudragit FS30D/guar gum doubled coated pellets have potential to deliver drug to the colon.更多还原